Identification of multiple 5-HT4 partial agonist clinical candidates for the treatment of Alzheimer's disease

…, DE Johnson, A Sawant-Basak…

文献索引：Brodney, Michael A.; Johnson, David E.; Sawant-Basak, Aarti; Coffman, Karen J.; Drummond, Elena M.; Hudson, Emily L.; Fisher, Katherine E.; Noguchi, Hirohide; Waizumi, Nobuaki; McDowell, Laura L.; Papanikolaou, Alexandros; Pettersen, Betty A.; Schmidt, Anne W.; Tseng, Elaine; Stutzman-Engwall, Kim; Rubitski, David M.; Vanase-Frawley, Michelle A.; Grimwood, Sarah Journal of Medicinal Chemistry, 2012 , vol. 55, # 21 p. 9240 - 9254

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被引用次数: 24

摘要

The cognitive impairments observed in Alzheimer's disease (AD) are in part a consequence of reduced acetylcholine (ACh) levels resulting from a loss of cholinergic neurons. Preclinically, serotonin 4 receptor (5-HT4) agonists are reported to modulate cholinergic function and therefore may provide a new mechanistic approach for treating cognitive deficits associated with AD. Herein we communicate the design and synthesis of potent, ...